Total synthesis of (-)-aplaminal

Org Lett. 2008 Oct 2;10(19):4363-5. doi: 10.1021/ol801794f. Epub 2008 Aug 28.

Abstract

The total synthesis and assignment of absolute configuration of (-)-aplaminal ( 1), a cytotoxic metabolite from a sea hare possessing a triazobicyclo[3.2.1]octane skeleton, has been achieved. The synthesis entailed condensation of a monoprotected diamine ( 3) with dimethyl 2-oxomalonate ( 4) to generate the imidazolidine core ( 2). Introduction of the third nitrogen via Mitsunobu activation and azide displacement, followed by reduction and lactam formation (AlMe 3), furnished (-)-aplaminal ( 1). Overall, the synthesis entailed 9 steps and proceeded in 19% overall yield.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Azabicyclo Compounds / chemical synthesis*
  • Azabicyclo Compounds / chemistry
  • Stereoisomerism

Substances

  • Azabicyclo Compounds
  • aplaminal